Background:
The rate-limiting step in the oral absorption of BCS class II drugs is dissolution.
Their low solubility is one of the major obstacles in the process of drug development. Dissolution
rate can be increased by decreasing the particle size to the nano range, eventually leading to increased
bioavailability.
Objective:
: In the present study, glimepiride loaded nanoparticles were prepared to enhance the dissolution
rate. The aim of the work was to examine the effect of polymer-drug ratio, solvent-antisolvent ratio and
speed of mixing on in vitro release of glimepiride.
Methods:
Glimepiride is an antidiabetic drug belonging to the BCS class II drugs. The polymeric nanoparticles
were formulated according to Box-Behnken Design (BBD) using nanoprecipitation technique. The
prepared nanoparticles were evaluated for in vitro drug release, loading capacity, entrapment efficiency,
and percentage yield.
Result:
It was found that NP-8 has maximum in vitro drug release and was selected as an optimized
batch. Analysis of Variance (ANOVA) was applied to the in vitro drug release to study the fitness and significance
of the model. The batch NP-8 showed 70.34 ± 1.09% in vitro drug release in 0.1 N methanolic
HCl and 92.02 ± 1.87% drug release in phosphate buffer pH 7.8. The release data revealed that the nanoparticles
followed zero order kinetics.
Conclusion:
The study revealed that the incorporation of glimepiride into gelucire 50/13 resulted in enhanced
dissolution rate.
Toward Biorelevant Dissolution: Application of a Biphasic Dissolution Model as a Discriminating Tool for HPMC Matrices Containing a Model BCS Class II Drug